Pharmacology Flashcards
What are examples of short acting β2 agonists?
Salbutamol (albuterol)
Terbutaline
Metoproterenol
Pirbuterol
What are examples of long acting β2 agonists?
Salmeterol
Formoterol
Vilanterol
What are the adverse effects of using Salbutamol?
- Skeletal muscle tremor
- Restlessness, apprehension
- Tachycardia & other arrhythmias
- Relaxation of pregnant uterus
What are anticholinergic agents/muscarinic agonists used in COPD and Asthma?
Ipratropium Bromide
Tiotropium
Umeclidinium
What is the mechanism of of action for β2 receptor agonists?
*stimulation of adenylate cyclase
*increase levels of cAMP, myosin light-chain kinase phosphorylation & inactivation
*relaxation of smooth m & bronchodilation
What is the mechanism of of action for Antichlolinergic?
Non-selective inhibition of acetylcholine at muscarinic (M 3) receptors on bronchial muscles —> relaxation of muscles
What are the adverse effects of using anticholinergic agents in the treatment of asthma?
Bronchitis
COPD exacerbation
Sinusitis
Dyspnoea
Headache
Flu-like symptoms
Dry mouth
What are the subdivisions of Bronchodilators?
β-agonists
Anticholinergic agents
Xanthine derivatives (Methylxanthines)
What type of drugs are Theophylline
Aminophylline, Pentoxifylline?
Methylxanthine Derivatives
Which methylxanthine drug is used in the treatment of Asthma?
Aminophylline
A- asthma
What are the mechanism of actions for Methlxanthine derivatives?
- Inhibit phosphodiesterase in bronchial muscle →accumulation of cAMP → relaxation of bronchial muscle via ↓ intracellular calcium & ↑ rate of inactivation of myosin light chain kinase
*Blocks adenosine receptors (A 1) . Resulting in disinhibition of adenylate cyclase, leading to ↑ cAMP → bronchodilation & tachycardia
Which subdivision of drugs are used as Anti-inflammatory agents in the treatment for Asthma and COPD?
*Glucocorticoids
*Mast cell stabilizers
*Inhibitors of leukotriene pathways
-Anti-leukotriene agents
-Leukotriene receptor antagonists
What is the treatment for Acute Streptococcus Pharyngitis?
Penicillin & Erythromycin
What can be used to treat Diphtheria?
Diphtheria antitoxin, Penicillin , Erythromycin
When are corticosteroids used in Asthma management?
*Systemic steroids used primarily when attack is severe
* Usually by inhalation - may reduce need for β2 agonist
Fill in the blank. _______ & ________ are examples of Oral corticosteroids?
Prednisone & Methylprednisolone
What are examples of Inhaled Corticosteroids?
Beware- Beclomethasone propionate
Beryllium -Budesonide
Money -Mometasone furorate
Truck - Triamcinolone acetonide
Coming - Ciclesonide
Fast- Flunisolide
Friday- Fluticasone propionate
” Beware Beryllium Money Truck Coming Fast Friday”
What classification of drugs inhibit Phospholipase A2 which causes a decrease in arachidonic and a decrease in prostaglandins and leuketrines?
Corticosteroids
Which drugs inhibit the 5-lipoxygenase pathway which catalyzes formation of leukotrienes from arachidonic acid?
Zileuton
Which drugs block the leuketrine D4 receptor (CysLTI)?
Montelukast & zafirlukast
Which drugs are best used to treat Aspirin induced and Exercise -Induced asthma?
Montelukast & zafirlukast
Which drug is a mast cell stabilizer that can be used in the treatment of Asthma?
Cromolyn / cromoglycate
Which drug is a monoclonal antibody that can be used in th treatment of Asthma?
Omalizumab
What are the major adverse effects of Leukotrine Inhibitors?
Neuropsychiatric effects, Headaches, GI distress, Hepatotoxity(Zileuton)
What are examples of Decongestants?
*Oxymetazoline
*Phenylephrine
*Pseudoephedrine
*Ephedrine
What is the mechanism of Decongestants?
Stimulate α-adrenergic receptors
- vasoconstriction of nasal vessels ↓ volume of nasal mucosa which causes opening of airways
What are the adverse effects of Decongestants?
*Hypertension
*Tachyarrhythmia
*Rebound nasal congestion with repeated topical use (via down-regulation of receptors?)
What type of drugs are used to treat Productive coughs?
Expectorants
What type of drugs are used to treat Non-Productive (dry) coughs?
Antitussives/cough suppressants
What are examples of Central acting Antitussives?
Opiates - Codeine
Dextromethorphan
Which central acting antitussive drug has mild opioid, ketamine,phencyclidine effect when used in excess and can cause an addictive state?
Dextromethorphan
Which peripheral active antitussives are described as Demulcents?
Honey, glycerin, licorice (use syrups or lozenges(sweetie)
What is another example of a peripheral acting antitussive ?
Humidifiers - ↓viscosity of bronchial secretions
Water may be inhaled as aerosol or as steam with/without medicaments e.g. eucalyptus, sodium chloride
What are some examples of Expectorants?
*Saline expectorants (e.g. potassium iodide, ammonium chloride, glycerol iodide, menthol)
*Guaifenesin
*Asmasol
What is the moa for Expectorants?
Stimulate receptors in the gastric mucosa which reflexly increase glandular secretion of the respiratory epithelium coating of mucosa + ease of removal of secretions
Bromhexine , Ambroxol & N-acetylcysteine are what type of drugs?
Mucolytics
Which drugs can be classified as First Generation Antihistamines
Diphenhydramine
Dimenhydrinate
Chlorpheniramine
Cyproheptadine
Cyclizine
Promethazine
What drugs can be classified as second generation antihistamines?
Laurie - Loratadine
Leys - Levocetirizine
Didn’t - Desloratidine
Come - Cetirizine
First- Fexofenadine
What is the moa for antihistamines?
*Competitively antagonize peripheral H1 receptors.
*Smooth m: antagonizes constricting action of histamine ( notably at bronchial & vascular smooth m)
*Capillaries: block ↑permeability that normally leads to oedema & wheal formation
What is the clinical use for antihistamines?
*Allergic reactions: symptomatic treatment of IgE hypersensitivity, allergic rhinitis, urticaria
*Motion sickness
*Sleep aids (OTC) “PM” preparations
What’s the difference between 1 st gen antihistamines and second gen antihistamines?
Second generation antihistamines causes less sedation than first generation.
